Serum testosterone suppression and potential for agonistic stimulation during chronic treatment with monthly depot formulation of domestic substitute of leuprorelin acetate microspheres for metastatic prostate cancer  

长期应用国产醋酸亮丙瑞林微球(单月剂型)治疗转移性前列腺癌时对血清睾酮的抑制和潜在刺激作用(英文)

作　　者：Dongliang Pan Liming Dong Lianchao Jin Bing Yang Zhe Zhou Kai Zhang Xianghua Zhang Ningchen Li 

机构地区：[1]Department of Urology,Peking University Shougang Hospital [2]Wujieping Urology Medical Center of Peking University [3]Department of Urology,Weihai Wendeng Center Hospital

出　　处：《The Chinese-German Journal of Clinical Oncology》2014年第7期320-322,共3页中德临床肿瘤学杂志（英文版）

基　　金：Supported by a grant from the State Key Laboratory of Environmental Chemistry and Ecotoxicology,Chinese Academy of Sciences(No.KF2011-12)

摘　　要：Objective： We aimed to evaluate the efficiency of serum testosterone suppression as well as the potential for agonistic stimulation of serum testosterone during chronic treatment with monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres for patients with metastatic prostate cancer. Methods： A total of 23 patients with metastatic prostate cancer were enrolled in the prospective study and received 6 monthly intramuscular depot injections of domestic substitute of leuprorelin acetate microspheres. Their levels and patterns of serum testosterone suppression and the potential for agonistic stimulation of serum testosterone were monitored following injection monthly （3.75 rag） depot formulation of domestic substitute of leuprorelin acetate microspheres for 24 weeks. Results： Mean testosterone was 431.4 ng/dL, 119.3 ng/dL, 28.2 ng/dL by week 1, 2, 3 and decreased to less than 15.6 ng/dL by week 4 where it remained throughout the treatment period. Median time to suppression of serum testosterone was 20.7 days. No transient minor ＂escape＂ from suppression occurred in all patients which was defined as a single testosterone value greater than 50 ng/dL once suppression was achieved. Assessment of agonistic stimulation following the second depot injection revealed no pattern of stimulation. Conclusion： We concluded that monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres could provide persistent, stable suppression of serum testosterone throughout the dosing intervals, and that the initial depot injection of this formulation also could provide sufficient pituitary desensitization to prevent agnostic stimulation of serum testosterone during chronic treatment.

关 键 词：prostatic neoplasms  metastatic TESTOSTERONE LEUPRORELIN domestic substitute 

分 类 号：R737.25[医药卫生—肿瘤]